Chemical Name:(RS)-a-Cyclopropyl-4-phosphonophenylglycine
Biological Activity:
Potent group II/III mGlu receptor
antagonist, with approximately 20-fold selectivity for group III over group II
(IC50 values of 2.2 and 46.2 nM respectively). A much less potent
antagonist at group I receptors in neonatal rat cortical slices (Kb
= 0.65 ± 0.07 nM).
Kemp et al (1996) α-Methyl-3-phosphonophenylglycine and α-cyclopropyl-4-phosphonophenylglycine
are potent antagonists at mGluRs negatively coupled to adenylyl cyclase.
Br.J.Pharmacol. (Abstr) 117 (in press). Toms et al (1996) The effects of (RS)-α-cyclopropyl-4-phosphonophenylglycine
((RS)-CPPG), a potent and selective metabotropic glutamate receptor antagonist.
BrJ.Pharmacol. 119 851. Janeet al (1996) Potent
antagonists at the L-AP4- and (1S3S)-ACPD-sensitive presynaptic metabotropic
glutamate receptors in the neonatal rat spinal cord. Neuropharmacology 35
1029
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
